Öner Sena, Kadı Abdulrahim, Tekman Enes, Kararenk Ayşe Cemre, Özer Elif Beyza, Ergin Kübra Nalkıran, Yuca Hafize, Arslan Mehmet Enes, Duman Resul, Şahin Aydan Acar, Pinar Nur Münevver, Atila Alptuğ, Bona Gülnur Ekşi, Karakaya Songül
Department of Molecular Biology and Genetics, Faculty of Science, Erzurum Technical University, Erzurum, Türkiye.
Department of Pharmaceutical Botany, Faculty of Pharmacy, Atatürk University, Erzurum, Türkiye.
Protoplasma. 2025 Jan 30. doi: 10.1007/s00709-025-02037-1.
Diabetes mellitus (DM) and cancer are multifactorial diseases with significant health consequences, and their relationship with aging makes them particularly challenging. Epidemiological data suggests that individuals with DM are more susceptible to certain cancers. This study examined the bioactive properties of Hypericum scabrum extracts, including methanol, hexane, and others, focusing on their inhibitory effects on key enzymes associated with DM and neurodegenerative diseases, such as acetylcholinesterase, butyrylcholinesterase, α-amylase, and α-glucosidase. Additionally, the impact of these extracts on human fibroblast (HDFa) and glioblastoma (U87MG) cancer cells was evaluated. The methanol extract was analyzed for elemental composition using ICP-MS, secondary metabolites, and amino acids via LC-MS/MS and underwent morphological and anatomical characterization. The methanol extract demonstrated notable inhibitory activity, with an IC value of < 1 µg/mL against α-glucosidase, surpassing acarbose in efficacy. The flower essential oil exhibited the highest inhibition (79.95%) of butyrylcholinesterase and the strongest acetylcholinesterase inhibition (21.62%). Elemental analysis revealed high concentrations of Na and K, while quinic acid and proline were identified as major metabolites, with proline concentrations reaching 494.0482 nmol/mL in the aerial part extract. The anticancer assays revealed higher cytotoxicity in U87MG glioblastoma cells compared to HDFa fibroblasts, suggesting potential applications for cancer therapy. The plant grows 20-50 cm tall, with yellow flowers and ovoid-ribbed capsules containing brown, reniform seeds. Its leaves are amphistomatic and ornamented, while stems feature striate cuticles and paracytic stomata. The pollen grains are microreticulate with syncolporate apertures. These results underscore the promising therapeutic potential of H. scabrum in managing DM, cancer, and neurodegenerative diseases, with its ability to inhibit key enzymes and show selective cytotoxicity against cancer cells.
糖尿病（DM）和癌症是具有重大健康后果的多因素疾病，它们与衰老的关系使其极具挑战性。流行病学数据表明，糖尿病患者更容易患某些癌症。本研究检测了糙叶金丝桃提取物的生物活性特性，包括甲醇提取物、己烷提取物等，重点关注其对与糖尿病和神经退行性疾病相关的关键酶的抑制作用，如乙酰胆碱酯酶、丁酰胆碱酯酶、α-淀粉酶和α-葡萄糖苷酶。此外，还评估了这些提取物对人成纤维细胞（HDFa）和胶质母细胞瘤（U87MG）癌细胞的影响。使用电感耦合等离子体质谱法（ICP-MS）分析甲醇提取物的元素组成，通过液相色谱-串联质谱法（LC-MS/MS）分析次生代谢物和氨基酸，并对其进行形态学和解剖学表征。甲醇提取物表现出显著的抑制活性，对α-葡萄糖苷酶的IC值<1μg/mL，疗效超过阿卡波糖。花精油对丁酰胆碱酯酶的抑制率最高（79.95%），对乙酰胆碱酯酶的抑制作用最强（21.62%）。元素分析显示钠和钾的浓度较高，同时奎尼酸和脯氨酸被确定为主要代谢物，地上部分提取物中脯氨酸浓度达到494.0482nmol/mL。抗癌试验表明，与HDFa成纤维细胞相比，U87MG胶质母细胞瘤细胞具有更高的细胞毒性，这表明其在癌症治疗方面具有潜在应用价值。该植物高20-50厘米，开黄花，有卵形肋状蒴果，内含棕色肾形种子。其叶两面有气孔且有纹饰，茎有条纹状角质层和副卫细胞气孔。花粉粒具微网状纹饰和联合孔。这些结果强调了糙叶金丝桃在治疗糖尿病、癌症和神经退行性疾病方面具有广阔的治疗潜力，它能够抑制关键酶并对癌细胞表现出选择性细胞毒性。
